Teverelix

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 571439

CAS#: 151272-78-5

Description: Teverelix is a water-soluble synthetic peptidic luteinizing hormone-releasing hormone (LHRH) antagonist. It suppresses luteinizing hormone and testosterone, with duration of effects depending on dosage.

Chemical Structure

img
Teverelix
CAS# 151272-78-5
Instruction

Theoretical Analysis

MedKoo Cat#: 571439
Name: Teverelix
CAS#: 151272-78-5
Chemical Formula: C74H100ClN15O14
Exact Mass: 1,457.73
Molecular Weight: 1,459.160
Elemental Analysis: C, 60.91; H, 6.91; Cl, 2.43; N, 14.40; O, 15.35

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: Teverelix

IUPAC/Chemical Name: D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N6-(aminocarbonyl)-D-lysyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-

InChi Key: NOENHWMKHNSHGX-IAOPALDYSA-N

InChi Code: InChI=1S/C74H100ClN15O14/c1-43(2)35-57(66(96)84-56(19-10-11-32-79-44(3)4)73(103)90-34-14-20-63(90)72(102)81-45(5)64(76)94)85-65(95)55(18-9-12-33-80-74(77)104)83-68(98)59(38-48-24-29-54(93)30-25-48)88-71(101)62(42-91)89-70(100)61(40-50-15-13-31-78-41-50)87-69(99)60(37-47-22-27-53(75)28-23-47)86-67(97)58(82-46(6)92)39-49-21-26-51-16-7-8-17-52(51)36-49/h7-8,13,15-17,21-31,36,41,43-45,55-63,79,91,93H,9-12,14,18-20,32-35,37-40,42H2,1-6H3,(H2,76,94)(H,81,102)(H,82,92)(H,83,98)(H,84,96)(H,85,95)(H,86,97)(H,87,99)(H,88,101)(H,89,100)(H3,77,80,104)/t45-,55-,56+,57+,58-,59+,60-,61-,62+,63+/m1/s1

SMILES Code: C[C@H](C(N)=O)NC([C@H]1N(C([C@H](CCCCNC(C)C)NC([C@H](CC(C)C)NC([C@@H](CCCCNC(N)=O)NC([C@H](CC2=CC=C(O)C=C2)NC([C@H](CO)NC([C@@H](CC3=CC=CN=C3)NC([C@@H](CC4=CC=C(Cl)C=C4)NC([C@@H](CC5=CC=C6C=CC=CC6=C5)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC1)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 1,459.16 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Erb K, Pechstein B, Schueler A, Engel J, Hermann R. Pituitary and gonadal endocrine effects and pharmacokinetics of the novel luteinizing hormone-releasing hormone antagonist teverelix in healthy men--a first-dose-in-humans study. Clin Pharmacol Ther. 2000 Jun;67(6):660-9. PubMed PMID: 10872648.

2: Schneider A, Lang A, Naumann W. Fluorescence spectroscopic determination of the critical aggregation concentration of the GnRH antagonists Cetrorelix, Teverelix and Ozarelix. J Fluoresc. 2010 Nov;20(6):1233-40. doi: 10.1007/s10895-010-0674-5. Epub 2010 Jun 1. PubMed PMID: 20514551.

3: Sorensen S, Rondeau JJ, Lenaerts V, Boutignon F, Wüthrich P, Deghenghi R, Adam A, Ong H. Radioimmunoassay of Antarelix, a luteinizing hormone releasing-hormone antagonist, in plasma and its application for pharmacokinetic study in dogs. J Immunoassay. 1996 Aug;17(3):205-26. PubMed PMID: 8842981.

4: Briant C, Ottogalli M, Morel M, Guillaume D. Use of a GnRH antagonist, antarelix, associated or not with hCG, to control ovulation in cyclic pony mares. Domest Anim Endocrinol. 2003 May;24(4):305-22. PubMed PMID: 12742549.

5: Mallardé D, Boutignon F, Moine F, Barré E, David S, Touchet H, Ferruti P, Deghenghi R. PLGA-PEG microspheres of teverelix: influence of polymer type on microsphere characteristics and on teverelix in vitro release. Int J Pharm. 2003 Aug 11;261(1-2):69-80. PubMed PMID: 12878396.

6: Briant C, Ottogalli M, Guillaume D. Attempt to control the day of ovulation in cycling pony mares by associating a GnRH antagonist with hCG. Domest Anim Endocrinol. 2004 Aug;27(2):165-78. PubMed PMID: 15219935.

7: Gonzalez-Bulnes A, Santiago-Moreno J, Garcia-Garcia RM, Souza CJ, Lopez-Sebastian A, McNeilly AS. Effect of GnRH antagonists treatment on gonadotrophin secretion, follicular development and inhibin A secretion in goats. Theriogenology. 2004 Apr 1;61(5):977-85. PubMed PMID: 14757481.

8: Gonzalez Añover P, Gonzalez-Bulnes A, Veiga-Lopez A, Garcia-Garcia RM, McNeilly AS, Encinas T. Effects of growth hormone and gonadotrophin releasing hormone antagonists on ovarian follicle growth in sheep. J Vet Pharmacol Ther. 2006 Oct;29(5):373-7. PubMed PMID: 16958781.

9: Gianotti L, Veldhuis JD, Destefanis S, Lanfranco F, Ramunni J, Arvat E, Marzetto M, Boutignon F, Deghenghi R, Ghigo E. Suppression and recovery of LH secretion by a potent and selective GnRH-receptor antagonist peptide in healthy early follicular-phase women are mediated via selective control of LH secretory burst mass. Clin Endocrinol (Oxf). 2003 Oct;59(4):526-32. PubMed PMID: 14510918.

10: Caraty A, Blomenröhr M, Vogel GM, Lomet D, Briant C, Beltramo M. RF9 powerfully stimulates gonadotrophin secretion in the ewe: evidence for a seasonal threshold of sensitivity. J Neuroendocrinol. 2012 May;24(5):725-36. doi: 10.1111/j.1365-2826.2012.02283.x. PubMed PMID: 22283564.

11: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Jun;29(5):359-73. PubMed PMID: 17805439.

12: Brüssow KP, Schneider F, Nürnberg G. Alteration of gonadotrophin and steroid hormone release, and of ovarian function by a GnRH antagonist in gilts. Anim Reprod Sci. 2001 Apr 30;66(1-2):117-28. PubMed PMID: 11343847.

13: Oussaid B, Lonergan P, Khatir H, Guler A, Monniaux D, Touze JL, Beckers JF, Cognie Y, Mermillod P. Effect of GnRH antagonist-induced prolonged follicular phase on follicular atresia and oocyte developmental competence in vitro in superovulated heifers. J Reprod Fertil. 2000 Jan;118(1):137-44. PubMed PMID: 10793635.

14: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2006 Jan-Feb;28(1):31-63. PubMed PMID: 16541195.

15: Guillaume D, Bruneau B, Briant C. Comparison of the effects of two GnRH antagonists on LH and FSH secretion, follicular growth and ovulation in the mare. Reprod Nutr Dev. 2002 May-Jun;42(3):251-64. PubMed PMID: 12405453.

16: Hinojosa AM, Bloeser JR, Thomson SR, Watson ED. The effect of a GnRH antagonist on endocrine and seminal parameters in stallions. Theriogenology. 2001 Sep 15;56(5):903-12. PubMed PMID: 11665891.

17: Odum J, Tinwell H, Jones K, Van Miller JP, Joiner RL, Tobin G, Kawasaki H, Deghenghi R, Ashby J. Effect of rodent diets on the sexual development of the rat. Toxicol Sci. 2001 May;61(1):115-27. PubMed PMID: 11294982.

18: Schneider F, Bellmann A, Becker F, Bambang Poernomo S, Rehfeldt C, Nürnberg G, Kanitz W. Gonadotropin release in periovulatory heifers after GnRH analogs measured by two types of immunoassays. Exp Clin Endocrinol Diabetes. 2002 Aug;110(5):235-44. PubMed PMID: 12148088.

19: Ashby J, Lefevre PA, Deghenghi R, Wallis N. Replacement of surgical castration by GnRH-inhibition or Leydig cell ablation in the male rat Hershberger antiandrogen assay. Regul Toxicol Pharmacol. 2001 Oct;34(2):188-203. PubMed PMID: 11603962.

20: Braun K, Kuhl P, Bernd M, Kutscher B. Stability of several LHRH antagonists against proteolytic enzymes and identification of degradation products by mass spectrometry. Pharmazie. 2001 Jan;56(1):45-9. PubMed PMID: 11210667.